Lornoxicam controlled release transdermal gel patch: Design, characterization and optimization using co-solvents as penetration enhancers.

The aim of the current study was to develop membrane-based transdermal patches of lornoxicam gel using oleic acid (OA)and propylene glycol (PG) as penetration enhancers to improve drug delivery across the skin and to evaluate in vivo analgesic and anti-inflammatory activity. For this purpose, nine formulations were developed in accordance with 32 factorial design using Design Expert® 11. The concentration of propylene glycol (X1) and oleic acid (X2) were selected as independent variable whereas Q10 (Y1), flux (Y2) and lag time (Y3) were considered as the response variables. The impact of drug loading, surface area, gel concentration, membrane variation and agitation speed on drug release and permeation was also studied. The skin sensitivity reaction, analgesic activity and anti-inflammatory action of the optimized patch were also determined in Albino Wistar rats. Stability studies were performed for three months at three different temperature conditions. The result suggests that a membrane-based system with controlled zero-order drug release of 95.8 ± 1.121% for 10 h exhibiting flux of 126.51±1.19 µg/cm2/h and lag time of 0.908 ±0.57h was optimized with the desired analgesic and anti-inflammatory effect can be obtained by using propylene glycol and oleic acid co-solvents as a penetration enhancer. The patch was also found stable at 4˚C for a period of 6.44 months. Formulation F9 comprising of 10% PG and 3% OA was selected as an optimized formulation. The study demonstrates that the fabricated transdermal system of lornoxicam can deliver the drug through the skin in a controlled manner with desired analgesic and anti-inflammatory activity and can be considered as a suitable alternative of the oral route.

Enteric coating of ibuprofen tablets (200 mg) using an aqueous dispersion system / Revestimento entérico dos comprimidos de ibuprofeno (200 mg), utilizando um sistema de dispersão aquosa

Ibuprofen is a propionic acid derivative that belongs to the class NSAIDs. Major adverse reactions associated with Ibuprofen are related to GIT and include peptic and mucosal ulcers, dyspepsia, severe gastric pain and bleeding, that results in excessive treatment failure. The goal of this study was to develop enteric coated ibuprofen tablets in order to avoid gastric mucosal irritation, diffusion of drug across mucosal lining and to let active ingredient be absorbed easily in small intestine. The formulation was developed and manufactured through the direct compression process, the simplest, easiest and most economical method of manufacturing. Enteric coating was done using an Opadry white subcoating and an aqueous coating dispersion of Acryl-Eze. Enteric coated formulation was subjected to disintegration and dissolution tests by placing in 0.1 M hydrochloric acid for 2 h and then 1 h in phosphate buffer with a pH of 6.8. About 0.04 percent of drug was released in the acidic phase and 99.05 percent in the basic medium. These results reflect that ibuprofen can be successfully enteric coated in order to prevent its release in the stomach and facilitate rapid release of the drug in the duodenum, due to the presence of superdisintegrant. Formulating this enteric coated tablets could increase patient compliance by decreasing adverse drug reactions (ADR S) associated with Ibuprofen therapy.

Ibuprofeno é um derivado do ácido propiônico, que pertence à classe dos fármacos não-esteróides (AINES). As principais reações adversas associadas com o ibuprofeno se referem àquelas do trato gastrintestinal (TGI), como úlceras pépticas e da mucosa, dispepsia, dor gástrica grave e sangramento, que resultam em muitas falhas de tratamento. O objetivo do estudo foi desenvolver comprimidos revestidos de ibuprofeno que impeçam a irritação da mucosa gástrica, difusão do fármaco através da mucosa e permitam, facilmente, a absorção do princípio ativo do intestino delgado. A formulação foi desenvolvida e manufaturada por meio de processo de compressão direta, método mais simples e econômico de preparação. O revestimento entérico foi efetuado utilizando-se subrevestimento com Opadry branco e revestimento por dispersão aquosa de Acryl-Eze. A formulação de revestimento para liberação entérica foi submetida a testes de desintegração e de dissolução, em ácido clorídrico 0,1 M, por 2 h, e, então, a h, em tampão fosfato pH 6,8. Cerca de 0,04 por cento do fármaco foi liberado na fase ácida e 99,05 por cento, no meio básico. Estes resultados refletem o fato de que o ibuprofeno pode ser revestido com sucesso, a fim de impedir sua liberação no estômago e facilitar a rápida liberação do fármaco no duodeno, devido à presença de superdesintegrante. A formulação de tais comprimidos aumentaria a adesão do paciente pela diminuição das reações adversas (RAs), associadas à terapia com ibuprofeno.

Formulation development and optimization of Ibuprofen tablets by direct compression method.

Ibuprofen is widely used as a prescription and non-prescription medicine. The aim of study is to prepare Ibuprofen tablets (200mg) using direct compression technique which is now days considered a cost effective and simple method of manufacturing. It is considered as an appropriate method for hygroscopic and thermolabile substances. In order to obtain the best, optimized product, nine different formulations were developed. Diluent (X1), disintegrant (X2) and lubricant (X3) were taken as independent variables. Weight variation (Y1), thickness (Y2), length and width (Y3), hardness (Y4), friability (Y5), disintegration (Y6), dissolution (Y7) and pharmaceutical assay (Y8) were studied as response variables. The results of all nine formulations were found within the acceptable limits conforming to those given in official compendia. However, F-6 was selected as an optimized product on the basis of high dissolution (99.05%) and Assay (100.04%). The variation of weight among the tablets of F-6 was least which showed best ratio of excipients in the formulation. Optimization has proven as an effective tool in product development. This is because no clear relationship exists between the variables.